| 词条 | Loxapine | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 408581688 | IUPAC_name = 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine | image = Loxapine.svg | width = 200px | image2 = Loxapine ball-and-stick model.png | width2 = 200px | tradename = Several trade names worldwide[1] | Drugs.com = {{drugs.com|monograph|loxapine-succinate}} | MedlinePlus = a682311 | DailyMedID = 50e11732-7387-452d-b3e6-db3a431d5c4a | licence_EU = yes | licence_US = Loxapine | pregnancy_US = C | legal_US = Rx-only | legal_AU = S4 | routes_of_administration = Oral, powder for inhalation | bioavailability = | protein_bound = 96.8%[2] | metabolism = Extensive hepatic; active metabolites include amoxapine and 8-hydroxyloxapine. Inhibits P-gp and is a substrate of CYP1A2, CYP3A4 and CYP2D6[2] | elimination_half-life = 4 hours (oral); 7.61 hours (inhalation) [2] | excretion = Majority are excreted within 24 hours, main route through urine (conjugated metabolites), small amounts through the feces (unconjugated metabolites) | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 1977-10-2 | ATC_prefix = N05 | ATC_suffix = AH01 | ATC_supplemental = | PubChem = 3964 | IUPHAR_ligand = 205 | DrugBank_Ref = {{drugbankcite|changed|drugbank}} | DrugBank = DB00408 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3827 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = LER583670J | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D02340 | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 50841 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 831 | C=18 | H=18 | Cl=1 | N=3 | O=1 | molecular_weight = 327.808 g/mol | SMILES = Clc2ccc1Oc4c(/N=C(\\c1c2)N3CCN(C)CC3)cccc4 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = XJGVXQDUIWGIRW-UHFFFAOYSA-N | melting_point = 109 | melting_high = 110 }}Loxapine (several trade names worldwide[1]) is a typical antipsychotic medication used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine. Several researchers have argued that loxapine may behave as an atypical antipsychotic.[2] Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant.[3] Medical usesThe US Food and Drug Administration (FDA) has approved loxapine inhalation powder for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults.[4] A brief review of loxapine found no conclusive evidence that it was particularly effective in patients with paranoid schizophrenia.[5] A subsequent systematic review considered that the limited evidence did not indicate a clear difference in its effects from other antipsychotics.[6] PrecautionsThis drug is unrelated to the habit-forming benzodiazepines, and misuse is rare.[7] The risks and side effect profile are comparable to other antipsychotics. Side effects{{further|Typical antipsychotic}}Note: Percentages given after possible adverse effects refer to the incidence of said adverse effects, according to DrugPoint.[2]
Pharmacology
The data in the table to the right was obtained from the PDSP Ki database and they are for binding towards human cloned proteins (receptor and transporter) unless otherwise specified.[11] See also
References1. ^1 Drugs.com [https://www.drugs.com/international/loxapine.html International names for loxapine] Page accessed March 3, 2016 2. ^{{cite journal |author=Glazer WM |title=Does loxapine have "atypical" properties? Clinical evidence |journal=The Journal of Clinical Psychiatry |volume=60 |issue=Suppl 10 |pages=42–6 |year=1999 |pmid=10340686}} 3. ^{{cite journal |vauthors=Cheung SW, Tang SW, Remington G |title=Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography |journal=Journal of Chromatography |volume=564 |issue=1 |pages=213–21 |date=March 1991 |pmid=1860915 |doi=10.1016/0378-4347(91)80083-O}} 4. ^Harrison, Pam: Inhalant Approved for Agitation in Bipolar I, Schizophrenia. Medscape. Dec 24, 2012. 5. ^{{cite journal |title=Clozapine and loxapine for schizophrenia |journal=Drug and Therapeutics Bulletin |volume=29 |issue=11 |pages=41–2 |date=May 1991 |pmid=1747161}} 6. ^{{cite journal |vauthors=Chakrabarti A, Bagnall A, Chue P, etal |title=Loxapine for schizophrenia |journal=Cochrane Database of Systematic Reviews |volume= |issue=4 |pages=CD001943 |year=2007 |pmid=17943763 |doi=10.1002/14651858.CD001943.pub2 |editor1-last=Chakrabarti |editor1-first=Abhijit}} 7. ^{{cite journal |doi=10.1056/NEJM198403013100920 |vauthors=Sperry L, Hudson B, Chan CH |title=Loxapine abuse |journal=The New England Journal of Medicine |volume=310 |issue=9 |pages=598 |date=March 1984 |pmid=6694719}} 8. ^1 2 3 4 5 6 Truven Health Analytics, Inc. DrugPoint® System (Internet) [cited 2013 Sep 21]. Greenwood Village, CO: Thomsen Healthcare; 2013. 9. ^Nordstrom K. Inhaled loxapine for rapid treatment of agitation in schizophrenia and bipolar disorder: an update. Neuropsychiatry [Internet]. 2012 Jun [cited 2013 Sep 21];2(3):253–60. Available from: {{Cite journal|title=Archived copy |journal=Neuropsychiatry |volume=2 |issue=3 |pages=253-260 |deadurl=yes |df= |doi=10.2217/npy.12.23 |year=2012 |last1=Nordstrom |first1=Kimberly }} 10. ^Taylor D, Paton C, Kapur S, Taylor D, South London and Maudsley NHS Trust. The Maudsley prescribing guidelines in psychiatry [Internet]. Chichester, West Sussex: John Wiley & Sons; 2012 [cited 2013 Sep 21]. Available from: http://site.ebrary.com/lib/uqat/Doc?id=10531429 11. ^1 {{cite web | title = PDSP Ki Database | website = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | format = HTML | accessdate = 14 August 2017 | url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=loxapine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}} 12. ^{{cite journal | vauthors = Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R | title = Interactions of recombinant human histamine H₁R, H₂R, H₃R, and H₄R receptors with 34 antidepressants and antipsychotics | journal = Naunyn Schmiedebergs Arch. Pharmacol. | volume = 385 | issue = 2 | pages = 145–70 | year = 2012 | pmid = 22033803 | doi = 10.1007/s00210-011-0704-0 | url = }} External links
| title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Dopamine receptor modulators}}{{Histamine receptor modulators}}{{Monoamine reuptake inhibitors}}{{Muscarinic acetylcholine receptor modulators}}{{Serotonin receptor modulators}} }}{{Tricyclics}} 4 : Chloroarenes|Dibenzoxazepines|Piperazines|Typical antipsychotics |
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